【摘要】 目的:研究盐酸哌唑嗪/羟丙基-β-环糊精的包合,寻找改善盐酸哌唑嗪制剂性能的方法。方法:采用紫外光谱法和相溶解度法研究盐酸哌唑嗪/羟丙基-β-环糊精包合作用。研磨法制备盐酸哌唑嗪/羟丙基-β-环糊精包合物,差示热分析验证包合物,紫外光谱法测定包合物的含量,并考察了包合物的稳定性。结果:盐酸哌唑嗪和羟丙基-β-环糊精的包合比为1∶1,包合常数为773 M-1。5%和10%羟丙基-β-环糊精可使盐酸哌唑嗪的溶解度分别增加16.9倍和23.6倍。3批包合物的平均含量为8.65%,盐酸哌唑嗪被包合后光稳定性增加。结论:羟丙基-β-环糊精包合可提高盐酸哌唑嗪的溶解度和光稳定性,该技术可用于改进盐酸哌唑嗪药物剂型。更多还原

【Abstract】 AIM:To study the inclusion complex of prazosin hydrochloride and HP-β-CD so as to improve the performance of prazosin hydrochloride formulation.METHODS:The inclusion complex of prazosin and HP-β-CD in aqueous solution was investigated by ultraviolet spectroscopy and phase solubility method;The inclusion complexes were prepared by milling and confirmed by DTA;The content of the inclusion complex was determined by ultraviolet spectroscopy and the stability of the inclusion complex was simultaneously analyzed.RESULTS:Prazosin hydrochloride formed complex with HP-β-CD with molar ratio of 1∶1 and the binding constant of 774 M^-1.The solubility of prazosin hydrochloride,in the presence of 5% and 10% HP-β-CD,was 16.9 and 23.6 times more than that alone.The average content of inclusion complex of three batches was 8.65%.Prazosin hydrochloride′s photo-stability was increased after complexed with HP-β-CD.CONCLUSION:HP-β-CD could improve the solubility and photo-stability of prazosin hydrochloride.It is feasible that HP-β-CD is used to improve the performance of prazosin hydrochloride formulation.更多还原